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1. 发明申请

WO2014079903A1 PHOSPHONUCLEOSIDES USEFUL IN THE TREATMENT OF VIRAL DISORDERS 审中-公开
标题翻译：用于治疗病毒性疾病的磷拮抗剂
公开(公告)号：WO2014079903A1
公开(公告)日：2014-05-30
申请号：PCT/EP2013/074321
申请日：2013-11-20
申请人： UNIVERSITY COLLEGE CORK , KATHOLIEKE UNIVERSITEIT LEUVEN
发明人： DEHAEN, Wim , BALZARINI, Jan , MAGUIRE, Anita , KEANE, Sarah Jane , FORD, Alan , MAGUIRE, Nuala , MULLINS, Nicholas, D.
IPC分类号： C07F9/6512 , C07F9/6561 , A61P31/12 , A61K31/675
CPC分类号： C07F9/65616 , A61K31/675 , A61K45/06 , C07F9/65121 , C07F9/65122 , C07F9/6561 , G01N33/573 , G01N2333/9128 , G01N2500/04 , G01N2500/20 , Y02A50/385
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, wherein the groups are as defined in the claims. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula (I), and the use of compounds of formula (I) in the preparation of a medicament for treating a viral disorder.
摘要翻译：本发明的第一方面涉及式（I）化合物或其药学上可接受的盐或前药，其中所述基团如权利要求中所定义。本发明的其它方面涉及包含式（I）化合物的药物组合物和式（I）化合物在制备用于治疗病毒性病症的药物中的用途。

2. 发明申请

WO2015177351A1 PHOSPHONATE NUCLEOSIDES USEFUL IN THE TREATMENT OF VIRAL DISEASES 审中-公开
标题翻译：用于治疗病毒性疾病的磷酸核苷
公开(公告)号：WO2015177351A1
公开(公告)日：2015-11-26
申请号：PCT/EP2015/061430
申请日：2015-05-22
申请人： UNIVERSITY COLLEGE CORK , KATHOLIEKE UNIVERSITEIT LEUVEN
发明人： MAGUIRE, Anita , FORD, Alan , BALZARINI, Jan , DEHAEN, Wim
IPC分类号： C07F9/38 , A61K31/675 , A61P31/12
CPC分类号： C07F9/65616 , C07F9/65121 , C07F9/65583
摘要： The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or prodrug thereof, and their use in medicine particular as anti-viral agents; wherein: Base is a natural or non-natural nucleobase, and the other substituents are as defined in the claims.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或前药，及其在药物中作为抗病毒剂的用途; 其中：碱是天然或非天然核碱基，其它取代基如权利要求中所定义。

3. 发明申请

WO2007129083A1 ANTI-VIRAL PYRIMIDINE NUCLEOSIDE DERIVATIVES 审中-公开
标题翻译：抗虚拟吡啶核苷衍生物
公开(公告)号：WO2007129083A1
公开(公告)日：2007-11-15
申请号：PCT/GB2007/001677
申请日：2007-05-09
申请人： UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED , KATHOLIEKE UNIVERSITEIT LEUVEN , MCGUIGAN, Christopher , BALZARINI, Jan , MIGLIORE, Marco
发明人： MCGUIGAN, Christopher , BALZARINI, Jan , MIGLIORE, Marco
IPC分类号： C07D491/04 , C07H19/04 , A61K31/70 , A61P31/12
CPC分类号： A61K31/7068 , A61K31/7052 , A61K31/706 , A61K31/7064 , C07D487/04 , C07D491/04 , C07D495/04
摘要： A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH 2 , Y is O, S or NH, Z is O, S or CH 2 , R 1 is C 1-6 alkyl, preferably n -alkyl, e.g., n -pentyl or n -hexyl, and one of R 2 and R 3 is OH, and the other of R 3 and R 2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R 2 or R 3 may be (IV): in which R 4 , R 5 , R 6 and R 7 are each independently H or C 1-2 alkyl. In preferred embodiments, one of R 2 or R 3 is valine, leucine, isoleucine or alanine, particularly valine.
摘要翻译：用于治疗或预防病毒感染的化合物，例如由水痘带状疱疹病毒引起的水痘或带状疱疹，所述具有通式（II）的化合物：其中X是O，S，NH或CH _{2，Y是O，S或NH，Z是O，S或CH 2，R 1是C 1-6，优选正烷基，例如正戊基或正己基，R 2和R 3中的一个是OH，另一个R' SUB 3和R 2是中性的，非极性的氨基酸部分或其药学上可接受的盐或水合物。所述中性，非极性氨基酸部分R 2或R 3可以是（Ⅳ）：其中R 4，R 3， R 5，R 6和R 7各自独立地为H或C 1-12烷基。在优选的实施方案中，R 2或R 3中的一个是缬氨酸，亮氨酸，异亮氨酸或丙氨酸，特别是缬氨酸。}

4. 发明申请

WO2013190137A2 NOVEL ANTI-CANCER COMPOUNDS 审中-公开
标题翻译：新型抗癌化合物
公开(公告)号：WO2013190137A2
公开(公告)日：2013-12-27
申请号：PCT/EP2013/063082
申请日：2013-06-21
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , UNIVERSITA DEGLI STUDI DI FERRARA
发明人： BALZARINI, Jan , DEHAEN, Wim , THOMAS, Joice , LIEKENS, Sandra , ROMAGNOLI, Romeo , BARALDI, Pier Giovanni
IPC分类号： C07D333/36
CPC分类号： C07D409/06 , A61K31/381 , A61K31/4436 , A61K45/06 , C07D307/54 , C07D307/66 , C07D333/36 , C07D333/38 , C07D401/12 , C07D405/12 , C07D409/04 , C07D409/12
摘要： The present invention relates to compounds having cytostatic activity against tumor cells. The compounds of the invention are of formula (I), or derivatives hereof, wherein R 0 , R 1 , R 2 , A, and X have defined meanings as described in claim 1.
摘要翻译：本发明涉及对肿瘤细胞具有抑制细胞活性的化合物。本发明的化合物具有式（I）或其衍生物，其中R 0，R 1，R 2，A和X具有如权利要求1中所述的含义。

5. 发明申请

WO2011085454A1 GP120 -BINDING BENZENE COMPOUNDS AND SACCHARIDE COMPOUNDS 审中-公开
标题翻译： GP120 -BINZENE化合物和SACCHARIDE化合物
公开(公告)号：WO2011085454A1
公开(公告)日：2011-07-21
申请号：PCT/BE2011/000001
申请日：2011-01-18
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN K.U.LEUVEN R&D , CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CSIC) , BALZARINI, Jan , CARRERO BERZAL, Paula , CASANOVA MALPICA, Elena , PEREZ PÉREZ, Ma Jesús , SAN-FÉLIX GARCÍA, Ana
发明人： BALZARINI, Jan , CARRERO BERZAL, Paula , CASANOVA MALPICA, Elena , PEREZ PÉREZ, Ma Jesús , SAN-FÉLIX GARCÍA, Ana
IPC分类号： C07C215/50 , C07C217/58 , C07C235/50 , C07C235/60 , C07H13/08 , A61K31/166 , A61K31/137 , A61K31/7024 , A61P31/18
CPC分类号： C07H13/08 , C07C215/50 , C07C215/78 , C07C217/58 , C07C217/84 , C07C235/50 , C07C235/60
摘要： The present invention provides for novel benzene compounds and saccharide compounds and for the use of said compounds for binding, titration (quantification), removing, purifying or separating the glycoprotein gp120, gp120 comprising viruses or cells infected with gp120 comprising viruses. The invention also provides for a method for the detection, binding, titration (quantification), removal, purification or separation of (or directing therapeutic or other agents to) gp120, gp120 comprising viruses or cells infected with gp120 comprising viruses. The invention further provides for the use of the compounds and for methods using the compounds for directing anti -viral drugs or other agents to gp120 comprising viruses or to gp120 comprising virus - infected cells. The present invention also provides processes for the preparation of said novel compounds.
摘要翻译：本发明提供新的苯化合物和糖类化合物，以及所述化合物用于结合，滴定（定量），除去，纯化或分离糖蛋白gp120，包含感染有包含病毒的gp120的病毒或细胞的gp120。本发明还提供了用于检测，结合，滴定（定量），去除，纯化或分离（或指导治疗剂或其它药剂）的gp120，gp120，其包含感染有包含病毒的gp120的病毒或细胞。本发明进一步提供了化合物的用途和使用该化合物将抗病毒药物或其它药剂引导至包含病毒的gp120或包含病毒感染细胞的gp120的方法。本发明还提供了制备所述新化合物的方法。

6. 发明申请

WO2009138507A2 ANTI-CANCER COMBINATION THERAPY 审中-公开
标题翻译：抗癌联合治疗
公开(公告)号：WO2009138507A2
公开(公告)日：2009-11-19
申请号：PCT/EP2009/055955
申请日：2009-05-15
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&D , BALZARINI, Jan , LIEKENS, Sandra
发明人： BALZARINI, Jan , LIEKENS, Sandra
CPC分类号： A61K45/06 , A61K31/513 , A61K31/7068 , A61K31/7076 , A61K2300/00
摘要： The present invention relates to a combination of therapeutic agents comprising: (a) a cytosine-based anti-cancer drug and/or a purine-based anticancer drug and (b) a therapeutic agent selected from the group consisting of thymidine phosphorylase inhibitors, and antibiotics against Mollicutes bacteria. The present invention also relates to the simultaneous, separate or sequential use of said combination for the treatment of cancer in mammals, especially in humans. The present invention also relates to methods of treatment of cancer, preferably in mammals infected with Mollicutes bacteria.
摘要翻译：本发明涉及治疗剂的组合，其包含：（a）基于胞嘧啶的抗癌药物和/或嘌呤类抗癌药物和（b）选自胸苷磷酸化酶抑制剂和抗生素对Mollicute细菌。本发明还涉及用于治疗哺乳动物，特别是人类中的癌症的所述组合的同时，分开或顺序使用。本发明还涉及治疗癌症的方法，优选在用Mollicutes细菌感染的哺乳动物中。

7. 发明申请

WO2015051422A1 NEW PRADIMICIN DERIVATIVES FOR THE TREATMENT OF DISEASES CAUSED BY KINETOPLASTIDS 审中-公开
标题翻译：用于治疗由药物引起的疾病的新型PRADIMICIN衍生物
公开(公告)号：WO2015051422A1
公开(公告)日：2015-04-16
申请号：PCT/BE2013/000055
申请日：2013-10-10
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , CONSEJO SUPERIOR DE INVESTIGACIONES CIENTÍFICAS - CSIC , TOYAMA PREFECTURE
发明人： BALZARINI, Jan , GONZÁLEZ PACANOWSKA, Dolores , RUI PÉREZ, Luis Miguel , CASTILLO ACOSTA, Víctor , IGARASHI, Yasuhiro
IPC分类号： A61K31/704 , A61P33/02
CPC分类号： A61K31/704 , Y02A50/409 , Y02A50/414 , Y02A50/415
摘要： The present invention relates to a class of novel pradimicins and analogues and derivatives thereof, including the compounds of formula A, I and 111, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof and their use to treat or prevent kinetoplastid infections and their use to manufacture a medicine to treat or prevent kinetoplastid infections, particularly infections with trypanosoma and leishmania, such as Trypanosoma brucei, Trypanosoma cruzi and Leischmania donovani. wherein R a , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as defined in the claim 1 or as described in detail in the description of the invention. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent kinetoplastid infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of kinetoplastid infections and pathologic conditions such as, but not limited to Trypanosomiasis, such as African trypanosomiasis, sleeping sickness, Chagas disease and leishmaniasis.
摘要翻译：本发明涉及一类新型的普拉德霉素及其类似物和衍生物，包括式A，I和111的化合物和/或其药学上可接受的加成盐和/或其立体异构体和/或其溶剂合物及其用于治疗或预防动粒细胞感染及其用于制造药物以治疗或预防巨细胞病毒感染，特别是锥虫和利什曼原虫的感染，例如布鲁斯锥虫，克氏锥虫和雷氏破乳杆菌（Leischmania donovani）。其中R a，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如权利要求1中所定义或如在本发明的描述中详细描述的。本发明还涉及所述化合物的药物组合物和所述药物组合物用于治疗或预防动粒细胞感染的用途。本发明还涉及所述化合物作为生物活性成分的用途，更具体地说是作为用于治疗动粒细胞感染和病理状况的药物，例如但不限于锥虫病，例如非洲锥虫病，睡眠病，恰加斯病和利什曼病。

8. 发明申请

WO2012034719A1 NOVEL ANTIVIRAL ACYCLIC NUCLEOSIDE PHOSPHONATES 审中-公开
标题翻译：新型抗氧化型核苷酸磷酸酯
公开(公告)号：WO2012034719A1
公开(公告)日：2012-03-22
申请号：PCT/EP2011/059090
申请日：2011-06-01
申请人： CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITE D'ORLEANS , KATHOLIEKE UNIVERSITEIT LEUVEN - K.U. LEUVEN R&D , AGROFOGLIO, Luigi, A. , ROY, Vincent , PRADERE, Hugo , BALZARINI, Jan , SNOECK, Robert , ANDREI, Graciela
发明人： AGROFOGLIO, Luigi, A. , ROY, Vincent , PRADERE, Hugo , BALZARINI, Jan , SNOECK, Robert , ANDREI, Graciela
IPC分类号： C07F9/6512 , C07F9/6561 , A61K31/675 , A61P31/12 , C07F9/6518
CPC分类号： A61K31/675 , A61K45/06 , C07F9/65121 , C07F9/65181 , C07F9/6561 , C07F9/65616
摘要： Compounds of formula (I) wherein A represents a nucleobase or a derivative thereof, n is equal to 0 or 1 and R', R" are carbonic chain, and R 10 is hydrogen or a carbonic chain for their use as antiviral agents.
摘要翻译：其中A表示核碱基或其衍生物的式（I）化合物，n等于0或1，R'，R“为碳链，R 10为氢或用作抗病毒剂的碳链。

9. 发明申请

WO2009030410A1 IMPROVEMENTS IN OR RELATING TO COMPOSITIONS FOR THE TREATMENT OR PROPHYLAXIS OF VIRAL INFECTIONS 审中-公开
标题翻译：治疗或预防感染组合物的改善或相关
公开(公告)号：WO2009030410A1
公开(公告)日：2009-03-12
申请号：PCT/EP2008/007009
申请日：2008-08-27
申请人： KATHOLIEKE UNIVERSITEIT LEUVEN , CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS , BALZARINI, Jan , CAMARASA, Maria Jose , VELAZQUEZ, Sonsoles
发明人： BALZARINI, Jan , CAMARASA, Maria Jose , VELAZQUEZ, Sonsoles
IPC分类号： C07K5/02 , C07K7/02 , A61K31/198 , C07H19/24 , A61K31/7068
CPC分类号： C07K9/003 , A61K47/542 , A61K47/64 , C07H19/24 , C07H23/00 , C07K5/0808
摘要： A compound of the general formula (III): wherein X is O, S, NH or CH 2 ; Y is O, S or NH; Z is O, S or CH 2 ; R 1 is C 1-8 alkyl, especially C 1-6 alkyl, preferably n -alkyl, e.g., n -pentyl or n -hexyl; at least one of R 2 and R 3 is H-[R 4 -R 5 ] n -R 6 -, in which: H-[R 4 -R 5 ] n - comprises an oligopeptide, R 4 being an amino acid and R 5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R 6 is a neutral, non-polar amino acid moiety that is bonded to R 5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R 3 and R 2 is H-[R 4 -R 5 ]n-R 6 - or H; or a pharmaceutically acceptable salt thereof.
摘要翻译：通式（III）的化合物：其中X是O，S，NH或CH 2; Y是O，S或NH; Z是O，S或CH 2; R1是C1-8烷基，特别是C1-6烷基，优选正烷基，例如正戊基或正己基; R2和R3中的至少一个是H- [R4-R5] n-R6-，其中：H- [R4-R5] n-包含寡肽，R4是氨基酸，R5是选自脯氨酸，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸，R6是中性，非极性氨基通过肽键与R5结合的酸部分，n为1,2,3,4或5; R3和R2中的另一个是H- [R4-R5] n-R6-或H; 或其药学上可接受的盐。

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